Journals / Turkish Journal of Chemistry / 2020 / Cilt: 44 - Sayı: 6

Design, synthesis, cytotoxic activity, and apoptosis inducing effects of 4-and N-substituted benzoyltaurinamide derivatives

Pages
1674–1693
Publication Date
2020-12-16
DOI
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

As a result, this study provides interesting data which can be used to design new taurine-based anticancer derivatives.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:In this study, a group of 4-substituted benzoyltaurinamide derivatives were designed, synthesized, and investigated for their anticancer activity against three cancer cell lines and one nontumorigenic cell line by MTT assay.
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Key Findings & Data:Among the final compounds, methoxyphenyl derivatives 14, 15, 16 were found to be effective against all the tested cancerous cell lines with promising selectivity.
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Conclusion & Impact:As a result, this study provides interesting data which can be used to design new taurine-based anticancer derivatives.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Apoptosis · Bcl-2 family proteins · caspase-3/9

Abstract

In this study, a group of 4-substituted benzoyltaurinamide derivatives were designed, synthesized, and investigated for their anticancer activity against three cancer cell lines and one nontumorigenic cell line by MTT assay. Among the final compounds, methoxyphenyl derivatives 14, 15, 16 were found to be effective against all the tested cancerous cell lines with promising selectivity. The most active compounds were further evaluated to determine the molecular mechanism of their anticancer activity by using western blot assay and the Annexin V-FITC/PI test. Compound 14 (in SH-SY5Y and MDA-MB-231 cell lines) and 15 (in SH-SY5Y cell line) were found to induce intrinsic apoptotic pathway by upregulating BAX, caspase-3, and caspase-9, while downregulating Bcl-2 and Bcl-xL expression levels. According to mechanistic studies, compounds displayed their anticancer activity via three different mechanisms: a. caspase-dependent, b. caspase-independent, and c. caspase-dependent pathway that excluded caspase-9 activation. As a result, this study provides interesting data which can be used to design new taurine-based anticancer derivatives.

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Cite This Article

AKGUL, O., ERDOGAN, M. A., BİRİM, D., KAYABASİ, C., GUNDUZ, C., ARMAGAN, G. (2020). Design, synthesis, cytotoxic activity, and apoptosis inducing effects of 4-and N-substituted benzoyltaurinamide derivatives. Turkish Journal of Chemistry, Cilt: 44 - Sayı: 6, 1674–1693. https://ajindex.com/articles/208805

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